1-苄基-4-(4-氟苯基)哌啶-4-醇合成路线 （共 8 条）
反应条件
1: 1-bromo-4-fluorobenzene With iodine; magnesium in tetrahydrofuran Grignard reaction; Inert atmosphereReflux; 2: 1-Phenylmethyl-piperidin-4-one in tetrahydrofuran T=20°C; Grignard reaction; 3 h; Inert atmosphereCooling with ice;
参考文献
Conway, Richard J.; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D.; Capuano, Ben; Crosby, Ian T.
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2560 - 2564
反应条件
in tetrahydrofuran; hexane; ethyl acetate
参考文献
Synaptic Pharmaceutical Corporation
Patent: US6159990 A1, 2000 ;
US 6159990 A
反应条件
1: 70 percent / dimethylformamide / 70 °C 2: 74 percent / tetrahydrofuran / 0 °C View Scheme
参考文献
Sakamuri, Sukumar; Enyedy, Istvan J; Kozikowski, Alan P; Zaman, Wahiduz A; Johnson, Kenneth M; Wang, Shaomeng
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 495 - 500
反应条件
1: 70 percent / dimethylformamide / 70 °C 2: 74 percent / tetrahydrofuran / 0 °C View Scheme
参考文献
Sakamuri, Sukumar; Enyedy, Istvan J; Kozikowski, Alan P; Zaman, Wahiduz A; Johnson, Kenneth M; Wang, Shaomeng
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 495 - 500
反应条件
palladium hydroxide on carbon; hydrogen in methanol
参考文献
NOVIRA THERAPEUTICS, INC.; HARTMAN, George D.; FLORES, Osvaldo A.
Patent: WO2013/96744 A1, 2013 ;
Location in patent: Page/Page column 213 ;
反应条件
1: 62 percent / p-toluenesulfonic acid monohydrate / toluene / 7 h / Heating 2: 77 percent / acetic acid; H2 / Pd/C / ethanol View Scheme
参考文献
Sakamuri, Sukumar; Enyedy, Istvan J; Kozikowski, Alan P; Zaman, Wahiduz A; Johnson, Kenneth M; Wang, Shaomeng
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 495 - 500
反应条件
hydrogenchloride; hydrogen; palladium on activated charcoal 1.) H2O, 2.) H2O, reflux; Multistep reaction;
参考文献
Bottcher; Barnickel; Hausberg; Haase; Seyfried; Eiermann
Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4020 - 4026
反应条件
1: 96 percent / trifluoroacetic acid / 1.5 h / Heating
2: 93 percent / 1,1,1-trichloro-ethane / 3 h / Heating
3: 93 percent / Zn (powder), acetic acid / H2O / 45 °C
View Scheme
参考文献
Perregaard; Moltzen; Meier; Sanchez
Journal of Medicinal Chemistry, 1995 , vol. 38, # 11 p. 1998 - 2008
